BR0212904A - Derivados substituìdos de 2-pirimidinil-6,7,8,9-tetraidropirimido-{1,2-a}pirimidin- 4-ona e 7-pirimidinil-2,3-diidroimidazo-{1,2-a}pirimi-din-5(1h)-on a para distúrbios neurodegenerativos - Google Patents
Derivados substituìdos de 2-pirimidinil-6,7,8,9-tetraidropirimido-{1,2-a}pirimidin- 4-ona e 7-pirimidinil-2,3-diidroimidazo-{1,2-a}pirimi-din-5(1h)-on a para distúrbios neurodegenerativosInfo
- Publication number
- BR0212904A BR0212904A BR0212904-3A BR0212904A BR0212904A BR 0212904 A BR0212904 A BR 0212904A BR 0212904 A BR0212904 A BR 0212904A BR 0212904 A BR0212904 A BR 0212904A
- Authority
- BR
- Brazil
- Prior art keywords
- group
- ring
- atom
- pyrimidinyl
- optionally substituted
- Prior art date
Links
- 208000015122 neurodegenerative disease Diseases 0.000 title abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 102000001267 GSK3 Human genes 0.000 abstract 2
- 108060006662 GSK3 Proteins 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- NFVJNJQRWPQVOA-UHFFFAOYSA-N n-[2-chloro-5-(trifluoromethyl)phenyl]-2-[3-(4-ethyl-5-ethylsulfanyl-1,2,4-triazol-3-yl)piperidin-1-yl]acetamide Chemical compound CCN1C(SCC)=NN=C1C1CN(CC(=O)NC=2C(=CC=C(C=2)C(F)(F)F)Cl)CCC1 NFVJNJQRWPQVOA-UHFFFAOYSA-N 0.000 abstract 2
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000004434 sulfur atom Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 101150053721 Cdk5 gene Proteins 0.000 abstract 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical group C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 abstract 1
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 1
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical group C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000001769 aryl amino group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000005678 ethenylene group Chemical group [H]C([*:1])=C([H])[*:2] 0.000 abstract 1
- 125000005677 ethinylene group Chemical group [*:2]C#C[*:1] 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002883 imidazolyl group Chemical group 0.000 abstract 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 abstract 1
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 230000003449 preventive effect Effects 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 150000008318 pyrimidones Chemical class 0.000 abstract 1
- 125000000168 pyrrolyl group Chemical group 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
- 125000003375 sulfoxide group Chemical group 0.000 abstract 1
- CXWXQJXEFPUFDZ-UHFFFAOYSA-N tetralin Chemical group C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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Abstract
"DERIVADOS SUBSTITUìDOS DE 2-PIRIMIDINIL-6,7,8,9-TETRAIDROPIRIMIDO-{1,2-A}PIRIMIDIN- 4-ONA E 7-PIRIMIDINIL-2,3-DIIDROIMIDAZO-{1,2-A}PIRIMI-DIN-5(1H)-ON A PARA DISTúRBIOS NEURODEGENERATIVOS". A invenção diz respeito a um derivado de pirimidona representado pela fórmula (1) ou um sal deste em que: X representa dois átomos de hidrogênio, um átomo de enxofre, um átomo de oxigênio ou um grupo C~ 1~-2~ alquila e um átomo de hidrogênio; Y representa uma ligação, um grupo etenileno, um grupo etinileno, um átomo de oxigênio, um átomo de enxofre, um grupo sulfonila, um grupo sulfóxido, um grupo carbonila, um átomo de nitrogênio sendo opcionalmente substituído; ou um grupo metileno opcionalmente substituído; R1 representa um grupo pirimidina opcionalmente substituído; R3 pode representar um grupo C~ 1~-6~ alquila opcionalmente substituido por um grupo C~ 6~-10~ arilóxi ou um C~ 6~-10~ arilamino; um grupo C~ 3~-6~, cicloalquila, um grupo C~ 1~-4~ alquiltio, um grupo C~ 1~-4~ alcóxi, um grupo C~ 1~-2~ alquila peralogenada, um grupo C~ 1~-3~ alquila halogenada, um grupo feniltio, um grupo benzila, um anel de benzeno, um anel de indano, um anel de 5,6,7,8-tetrahidronaftaleno, um anel de naftaleno, um anel de piridina, um anel de pirrol, um anel de tiofeno, um anel de furano ou um anel de imidazol; R3 e R4 representam cada um, independentemente, um átomo de hidrogênio, grupo C~ 1~-6~ alquila, um grupo hidróxi, um grupo C~ 1~-4~ alcóxi ou um átomo de halogênio; R5 representa um átomo de hidrogênio, um grupo C~ 1-6~ alquila ou um átomo de halogênio. A invenção também diz respeito a um medicamento compreendendo o dito derivado ou um sal deste como um ingrediente ativo que é usado para o tratamento preventivo e/ou terapêutico de uma doença neurodegenerativa causada por atividade normal de GSK3<225>3 OU GSK3<225>3 E cdk5/p25, como doença de alzheimer.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01402431A EP1295884A1 (en) | 2001-09-21 | 2001-09-21 | 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]Pyrimidin-4-one and 7-Pyrimidinyl-2,3-Dihydroimidazo[1,2-a]Pyrimidin-5(1H)one derivatives |
| EP02290488A EP1340760A1 (en) | 2002-02-28 | 2002-02-28 | Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)one derivatives |
| PCT/EP2002/011127 WO2003027115A1 (en) | 2001-09-21 | 2002-09-19 | Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1h)one derivatives for neurodegenerative disorders |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR0212904A true BR0212904A (pt) | 2004-10-13 |
Family
ID=26077255
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR0212904-3A BR0212904A (pt) | 2001-09-21 | 2002-09-19 | Derivados substituìdos de 2-pirimidinil-6,7,8,9-tetraidropirimido-{1,2-a}pirimidin- 4-ona e 7-pirimidinil-2,3-diidroimidazo-{1,2-a}pirimi-din-5(1h)-on a para distúrbios neurodegenerativos |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US7388005B2 (pt) |
| EP (1) | EP1430056B1 (pt) |
| JP (2) | JP4570361B2 (pt) |
| KR (1) | KR100868840B1 (pt) |
| CN (1) | CN1247586C (pt) |
| AR (1) | AR036599A1 (pt) |
| AT (1) | ATE307815T1 (pt) |
| AU (1) | AU2002342798C1 (pt) |
| BR (1) | BR0212904A (pt) |
| CA (1) | CA2457952C (pt) |
| CY (1) | CY1105553T1 (pt) |
| DE (1) | DE60206946T2 (pt) |
| DK (1) | DK1430056T3 (pt) |
| EA (2) | EA009456B1 (pt) |
| ES (1) | ES2250721T3 (pt) |
| HU (1) | HUP0500332A3 (pt) |
| IL (2) | IL160397A0 (pt) |
| MX (1) | MXPA04002632A (pt) |
| NO (1) | NO329566B1 (pt) |
| NZ (1) | NZ531244A (pt) |
| PL (1) | PL370535A1 (pt) |
| SI (1) | SI1430056T1 (pt) |
| WO (1) | WO2003027115A1 (pt) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1454909B1 (en) * | 2003-03-07 | 2008-08-20 | Sanofi Aventis | 8'-pyridinyl-dihydrospiro- (cycloalkyl) -pyrimido (1,2-a) pyrimidin-6-one and 8'-pyrimidinyl-dihydrospiro (cycloalkyl) -pyrimido (1,2-a) pyrimidin-6-one derivatives and their use against neurodegenerative diseases |
| EP1557417B1 (en) * | 2003-12-19 | 2007-03-07 | Sanofi-Aventis | Substituted 8'-pyri(mi)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a] pyrimidin-6-one derivatives |
| WO2005070932A2 (en) | 2004-01-22 | 2005-08-04 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| JP2008543840A (ja) * | 2005-06-14 | 2008-12-04 | シェーリング コーポレイション | アスパルチルプロテアーゼインヒビター |
| EP2258358A3 (en) | 2005-08-26 | 2011-09-07 | Braincells, Inc. | Neurogenesis with acetylcholinesterase inhibitor |
| EP1928437A2 (en) | 2005-08-26 | 2008-06-11 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation |
| EP1940389A2 (en) | 2005-10-21 | 2008-07-09 | Braincells, Inc. | Modulation of neurogenesis by pde inhibition |
| US20070112017A1 (en) | 2005-10-31 | 2007-05-17 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
| US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
| AU2007249399A1 (en) | 2006-05-09 | 2007-11-22 | Braincells, Inc. | Neurogenesis by modulating angiotensin |
| US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
| EP1939187A1 (en) | 2006-12-20 | 2008-07-02 | Sanofi-Aventis | Substituted heteroaryl pyridopyrimidone derivatives |
| EP1992621A1 (en) * | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Heteroarylamide-substituted pyrimidone derivatives for the treatment of neurodegenerative diseases |
| EP1992624A1 (en) * | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Heteroarylamide pyrimidone compounds |
| EP1992625A1 (en) | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Arylamide pyrimidone compounds |
| EP1992620A1 (en) * | 2007-05-16 | 2008-11-19 | Sanofi-Aventis | Arylamide pyrimidone derivatives for the treatment of neurodegenerative diseases |
| EP2085400A1 (en) * | 2008-01-29 | 2009-08-05 | Sanofi-Aventis | Substituted heteroarylamide oxazepinopyrimidone derivatives |
| EP2090579A1 (en) * | 2008-01-29 | 2009-08-19 | Sanofi-Aventis | Substituted heteroarylamide diazepinopyrimidone derivatives |
| EP2085399A1 (en) * | 2008-01-29 | 2009-08-05 | Sanofi-Aventis | substituted arylamide oxazepinopyrimidone derivatives |
| EP2090578A1 (en) * | 2008-01-29 | 2009-08-19 | Sanofi-Aventis | Substituted arylamide diazepinopyrimidone derivatives for the treatment of neurodegenerative diseases caused by abnormal activity of GSK3-beta |
| EP2138485A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted N-Oxide pyrazine derivatives |
| EP2138498A1 (en) * | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted tricyclic derivatives against neurodegenerative diseases |
| EP2138493A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted pyrimidone derivatives |
| EP2138494A1 (en) * | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted alkyl pyrimidin-4-one derivatives |
| EP2138492A1 (en) | 2008-06-26 | 2009-12-30 | Sanofi-Aventis | Substituted pyrimidin-4-one derivatives |
| EP2138488A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | 4-(pyridin-4-yl)-1H-[1,3,5]triazin-2-one derivatives as GSK3-beta inhibitors for the treatment of neurodegenerative diseases |
| EP2138495A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | Substituted pyrimido[2,1-a]isoquinolin-4-one derivatives |
| WO2010099217A1 (en) | 2009-02-25 | 2010-09-02 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
| US8421890B2 (en) | 2010-01-15 | 2013-04-16 | Picofield Technologies, Inc. | Electronic imager using an impedance sensor grid array and method of making |
| US20170165230A1 (en) | 2014-04-09 | 2017-06-15 | Christopher Rudd | Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity |
| JP7403351B2 (ja) | 2020-02-27 | 2023-12-22 | 三菱重工業株式会社 | 通信ポイント決定装置、通信ポイント決定方法およびプログラム、並びに点検システム |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3865836A (en) * | 1972-12-08 | 1975-02-11 | Janssen Pharmaceutica Nv | Bicyclic imidazoles |
| SU600143A1 (ru) * | 1976-12-06 | 1978-03-30 | Ордена Трудового Красного Знамени Институт Органического Синтеза Ан Латвийской Сср | Способ получени гетероциклических систем, содержащих бормзамещенный имидазол |
| JPS63216886A (ja) * | 1987-03-05 | 1988-09-09 | Sumitomo Chem Co Ltd | ピリミドピリミジン誘導体およびその製造法 |
| JP2862958B2 (ja) * | 1990-06-09 | 1999-03-03 | 三協化学株式会社 | 感熱転写記録用色素 |
| AU4920397A (en) | 1996-10-11 | 1998-05-11 | Chiron Corporation | Purine inhibitors of glycogen synthase kinase 3 (gsk3) |
| IL130181A0 (en) | 1996-12-05 | 2000-06-01 | Amgen Inc | Substituted pyrimidone and pyridone compounds and methods of use |
| BR9908004A (pt) * | 1998-02-17 | 2001-12-18 | Tularik Inc | Composto, composição e método para prevençãoou supressão de uma infecção viral |
| CN100335479C (zh) * | 1999-12-17 | 2007-09-05 | 希龙公司 | 糖元合成酶激酶3的双环抑制剂 |
| FR2804959B1 (fr) * | 2000-02-15 | 2006-04-28 | Centre Nat Rech Scient | Utilisation de derives de paullones pour la fabrication de medicaments |
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